CN105769841A - Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination - Google Patents
Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination Download PDFInfo
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- CN105769841A CN105769841A CN201610155201.8A CN201610155201A CN105769841A CN 105769841 A CN105769841 A CN 105769841A CN 201610155201 A CN201610155201 A CN 201610155201A CN 105769841 A CN105769841 A CN 105769841A
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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Abstract
The invention discloses an application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing a drug for pregnancy termination and belongs to the technical field of medicines. The drug is prepared from an active ingredient and pharmaceutically acceptable adjuvants, and the active ingredient comprises syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid only. The drug has high efficiency of pregnancy termination, is harmless to organs, low in toxic and side effect, safe and reliable, and is applicable to termination of early pregnancy.
Description
The application be applicant Qingdao Hua Zhicao Pharmaceutical Technology Co., Ltd, fourth peak propose application for a patent for invention (invention entitled: a kind of medical composition and its use for terminal pregnancy, Application No.: 2014103939365, filing date: on August 12nd, 2014) divisional application.
Technical field
The invention belongs to pharmaceutical technology field, in particular to syringic acid/4-hydroxyl-3,5-dimethoxybenzoic acid purposes in preparation is used for the medicine of terminal pregnancy.
Background technology
It is known that in daily life, not using effective contraceptives to cause the thing of Women of childbearing age unexpected pregnancy to happen occasionally due to men and women, unexpected pregnancy once occurs, it is necessary to take in a short time extremely to amass effective measures terminal pregnancy.At present, domestic terminal pregnancy mainly uses operation or medicine by embryo from utero discharging, and reaches to terminate the purpose of behavior of unwanted pregnant；In the annual about 10,000,000 person-times ground induced abortion of China.
At present, adding, with mifepristone, the method that Misoprostol drug oral terminates early pregnancy, this is China's topmost Western medicine expiration Pregnancy Methods.The women doing expiration gestation first has to take mifepristone 1500mg and takes Misoprostol 600Ug again after 48 hours.There is pain in secondary uterine contractile, belly, and most discharge embryos in 6 hours, minority was discharged in one week.If row is not clean, may proceed to gestation, also need to carry out apparatus manual termination gestation.During terminal pregnancy, in addition to hypogastralgia.There is vomiting, diarrhoea and heating paresthesia in some patient.After expiration gestation, amount of bleeding is more, average 10-15 days of bleeding time.For being busy with one's work, the patient cannot fully having a rest after terminal pregnancy, can cause anaemia, infection and the unnecessary trouble such as dilatation and curettage again because of bleeding time length, terminal pregnancy failure.Cycle stratigraphy can cause functional disturbances of gastrointestinal tract, the symptom such as nausea,vomiting,diarrhea, stomachache occurs, also can cause angiocardiopathy.Expiration gestation is suitable only for menelipsis pregnant woman within 49 days, efficient up to about 90%.But also there are many expiration gestation persons not exclusively massive haemorrhage to occur because terminal pregnancy, threat to life, and easily cause that women's is infertile, especially to repeatedly terminal pregnancy person.
It is to use injection of pituitrin and ergometrine that another kind Western medicine carries out the method for expiration gestation, easily causes elevation of the blood pressure, and induces angina pectoris, allergic reaction, palpitaition occurs, breathes hard, even cause anaphylactic shock.Also somebody use quinine to carry out expiration gestation, headache, tinnitus, dim eyesight, vomiting, eyesight and dysacousis often occur, severe patient can cause body temperature, drop in blood pressure, last respiratory paralysis and dead.Rivanol, root of Chinese trichosanthes, overgrown with weeds flower preparation, prostaglandin, hypertonic saline etc. is used to carry out expiration gestation, it is adaptable to 12-24 week is without contraindication person.A period of time after medication, uterus battle array contracting can be caused to force cervical dilatation, discharge fetus and placenta.Route of administration has the inside and outside injection of amniotic cavity, intramuscular injection and vagina to place, and these approach are different because selecting medicine different.But its terminal pregnancy rate is relatively low, and easily pregnant woman is caused danger.Also somebody has an abortion with various cathartics, and due to diarrheal dehydration, severe patient causes electrolyte disturbance, arrhythmia cordis, shock, Acute renal failure.
In sum, it is the highest generally to there is terminal pregnancy rate in current expiration gestation, easily causes various side effect, the problem of the serious life security even having influence on pregnant woman.
Summary of the invention
It is an object of the invention to provide a kind of novel medicine for terminal pregnancy.This medicine is active component with syringic acid/4-hydroxyl-3,5-dimethoxybenzoic acid, can be used for the termination of early pregnancy.
The object of the present invention is achieved like this:
A kind of pharmaceutical composition for terminal pregnancy, is prepared from by active component and pharmaceutically acceptable auxiliary material, and described active component includes syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid).
Preferably, being previously discussed for the pharmaceutical composition of terminal pregnancy, wherein said active component is made up of as sole component syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid).
Pharmaceutical composition for terminal pregnancy of the present invention, wherein syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) carry out relevant animal test as active component in gavage mode, result medicine is notable through gastrointestinal absorption, and therefore described pharmaceutical composition can be oral formulations.Wherein said oral formulations includes tablet, capsule, granule.
It should be noted that, common process according to formulation art, those skilled in the art is easy to the oral formulations that syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) and acceptable auxiliary material in pharmacy are prepared as commonly use, such as oral liquid, granule, tablet, capsule.Wherein, in pharmacy, acceptable auxiliary material includes filler, disintegrant, adhesive, flavouring, lubricant etc..Described filler is selected from following one or more: pregelatinized starch, lactose, mannitol and microcrystalline cellulose；Described disintegrant is selected from following one or more: sodium carboxymethyl starch, PVPP, Ac-Di-Sol and low-substituted hydroxypropyl cellulose；Described adhesive is selected from following one or more: starch slurry, hydroxypropyl cellulose solution, povidone solution；Described lubricant is selected from following one or both: magnesium stearate, talcum powder.
In reproductive process, embryonated egg through the process such as implantation, differentiation, finally develops into a ripe fetus in maternal uterine.The process of blastocyst cytula implanted device Endometrium is referred to as implantation.Mouse post-coitum cytula runs 3d in fallopian tubal, enters uterus and start to implant after 4-5d.At pregnant the 3-4 days, the present inventor gives syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) gavage carry out gestation intervention, control group gives physiological saline gavage, put to death mouse after gestation 12d and dissect, finding that heavy dose of syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) can make mouse implantation inhibiting rate reach more than 80%, this prompting syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) has obvious Antiimplantation Action.And increase with dosage, the inhibitory action of implantation is also remarkably reinforced.Based on above result of study, the present invention also provides for a kind of pharmaceutical applications, it may be assumed that syringic acid-(4-hydroxyl-3, the 5-dimethoxybenzoic acid) purposes in preparation is used for the medicine of terminal pregnancy.
Compared with prior art, the pharmaceutical composition containing syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) that the present invention relates to has following prominent advantage: the efficiency of (1) terminal pregnancy is high, and simultaneously to internal organs fanout free region, toxic and side effect is little；(2) it is that terminal pregnancy provides new drug candidate, it is adaptable to early pregnancy terminates.
Detailed description of the invention
Cloudy bolt (Vaginal plug) be some rodent at post-coitum, a kind of stock white fluidity material formed immediately, be blocked in vagina in Cervical chamber.Being the one mark checking the most no mating of animal, the same day that will appear from cloudy bolt calculates as pregnant 1st day.It is that the secretion by male mouse seminal vesicle and solidification gland is at the concretionary product of vagina.Small white mouse is typically formed in post-coitum 4-5min.Big cloudy bolt can protrude from introitus, little in vagina or cervix, needs to open introitus and just can look into and see.Cloudy bolt typically softens gradually at post-coitum 1h, comes off after 16-24h.But also have and only exist 4-5h, and more than most existed 48h.In reproductive process, embryonated egg through the process such as implantation, differentiation, finally develops into a ripe fetus in maternal uterine.The process of blastocyst cytula implanted device Endometrium is referred to as implantation.Mouse post-coitum cytula runs 3d in fallopian tubal, enters uterus and start to implant after 4-5d.At pregnant the 3-4 days, the present inventor gives syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) gavage carry out gestation intervention, control group gives physiological saline gavage, put to death mouse after gestation 12d and dissect, finding that heavy dose of syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) can make mouse implantation inhibiting rate reach more than 80%, this prompting syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) has obvious Antiimplantation Action.And increase with dosage, the inhibitory action of implantation is also remarkably reinforced.
The following is concrete process of the test:
Healthy mature Kunming mouse, body weight 25-35g, female 100, male 50, give normal diet and cleaning running water.Mouse mates with male and female 2:1, and every morning checks vagina, opens vaginal orifice with pincet, and the female mouse that will appear from cloudy bolt is taken out, and as the 1st day of gestation, is grouped raising by date.Pregnant mouse is randomly divided into following four groups: blank group, syringic acid-(4-hydroxyl-3,5-dimethoxybenzoic acid) basic, normal, high dosage group (2,6,18mg/kg).At pregnant the 3-4 days, on the basis of weight, low, medium and high dosage group gives syringic acid-(4-hydroxyl-3, the 5-dimethoxybenzoic acid) of corresponding dosage, 0.1ml/10g gavage, and control group gives physiological saline 0.1ml/10g gavage, every day 1 time.5h after gestation is administered on the 12nd day, puts to death mouse cervical dislocation, dissects, observe the embryo number in uterus, calculate antipregnancy rate (antipregnancy rate=non-animal pregnancy number/animal used as test number × 100%)；Take out ovary, adrenal gland, spleen, thymus gland, weigh and calculate its organ index (organ index=internal organs weight in wet base/body weight × 100).
Dissecting each group of experiment mice, find that blank group and low dosage administration group Pregnant Mouse Uterus diameter are thick, flesh pink, glossy, the embryo of cornua uteri is beading, is evenly distributed, and embryonic development is good；Middle and high dosed administration group non-Pregnant Mouse Uterus diameter is substantially little than control group, has no embryonic development.Antipregnancy rate comparative result between each group is shown in Table 1.It addition, each administration group compares no significant difference with blank group organ index, the results are shown in Table 2.
Table 1 is respectively organized female mouse implantation situation and is compared
Table 2 is respectively organized mice organs index and is compared
Claims (5)
1. syringic acid/4-hydroxyl-3,5-dimethoxybenzoic acid purposes in preparation is used for the medicine of terminal pregnancy, it is characterized in that: the described medicine for terminal pregnancy is prepared from by active component and pharmaceutically acceptable auxiliary material, described active component is made up of as sole component syringic acid/4-hydroxyl-3,5-dimethoxybenzoic acid.
Purposes the most according to claim 1, it is characterised in that: the described medicine for terminal pregnancy is oral formulations.
Purposes the most according to claim 2, it is characterised in that: described oral formulations is oral liquid, tablet, capsule or granule.
Purposes the most according to claim 1, it is characterised in that: in described pharmacy, acceptable auxiliary material includes filler, disintegrant, adhesive, flavouring, lubricant.
Purposes the most according to claim 4, it is characterised in that: described filler is selected from following one or more: pregelatinized starch, lactose, mannitol and microcrystalline cellulose；Described disintegrant is selected from following one or more: sodium carboxymethyl starch, PVPP, Ac-Di-Sol and low-substituted hydroxypropyl cellulose；Described adhesive is selected from following one or more: starch slurry, hydroxypropyl cellulose solution, povidone solution；Described lubricant is selected from following one or both: magnesium stearate, talcum powder.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610155201.8A CN105769841A (en) | 2014-08-12 | 2014-08-12 | Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination |
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| CN201610155201.8A CN105769841A (en) | 2014-08-12 | 2014-08-12 | Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination |
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| CN201410393936.5A Division CN104127398B (en) | 2014-08-12 | 2014-08-12 | A kind of medical composition and its use for termination of pregnancy |
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| CN105769841A true CN105769841A (en) | 2016-07-20 |
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| CN201610155201.8A Withdrawn CN105769841A (en) | 2014-08-12 | 2014-08-12 | Application of syringic acid/4-hydroxy-3,5-dimethoxybenzoic acid in preparing drug for pregnancy termination |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109316475A (en) * | 2018-10-22 | 2019-02-12 | 中国人民解放军第二军医大学第二附属医院 | Syringic acid/3,5- dimethoxy-4 '-hydroxybenzoic acid promotes the application in neural restoration drug in preparation |
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| CN1843345A (en) * | 2005-06-07 | 2006-10-11 | 江中药业股份有限公司 | 1,5-di-o-caffenoylquinate solid formulation and its preparation method |
| CN102114001A (en) * | 2009-12-30 | 2011-07-06 | 北京德众万全医药科技有限公司 | Orally administered solid preparation containing tolvaptan |
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2014
- 2014-08-12 CN CN201610155201.8A patent/CN105769841A/en not_active Withdrawn
Patent Citations (4)
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| CN1843345A (en) * | 2005-06-07 | 2006-10-11 | 江中药业股份有限公司 | 1,5-di-o-caffenoylquinate solid formulation and its preparation method |
| CN102114001A (en) * | 2009-12-30 | 2011-07-06 | 北京德众万全医药科技有限公司 | Orally administered solid preparation containing tolvaptan |
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| JOGEN CHANDRA KALITA等: "Anti-fertility effects of the methanolic root extract of Careya arborea Roxb in albino mice", 《THE BIOSCAN》 * |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109316475A (en) * | 2018-10-22 | 2019-02-12 | 中国人民解放军第二军医大学第二附属医院 | Syringic acid/3,5- dimethoxy-4 '-hydroxybenzoic acid promotes the application in neural restoration drug in preparation |
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Inventor after: Yu Houmei Inventor after: Ding Feng Inventor before: Ding Feng |
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Application publication date: 20160720 |